C4. Antifungal agents Flashcards
What is the MOA of Amphotericin B?
Binds ergosterol and forms pores in fungal cell membrane.
What are the indications for caspofungin?
- Invasive aspergillosis
What are the side effects of Anidulafungin?
- May cause HA release on infusion → flushing.
What are the side effects of micafungin?
- Increases risk of hepatic cancer
- Suppresses bone marrow
What is the MOA of Flucytosine?
converted into 5-fluorouracil → halts DNA/RNA synthesis.
What are the SE of Flucytosine?
- Bone marrow suppression
- Hepatotoxicity
- May cause toxic enterocolitis at high doses
What is the MOA of Nystatin?
Same as amphotericin, binds ergosterol and forms pores in fungal cell membrane.
What is the MOA of Azoles?
Azoles inhibit ergosterol synthesis from lanosterol via fungal CYP450 (14-alpha demethylase).
List the First Generation Triazoles?
- Fluconazole
- Itraconazole
What are the indications for Itraconazole?
- Good for dimorphic fungi (Histo, Blasto, Coccidio, Sporothrix) and for onychomycosis and dermatophytosis (tinea) … remember T drugs for tinea (Keto-/Clotrim-/Itraconazole, Terbinafine)
- Also effective in Aspergillus infections.
What are the indications for Fluconazole?
- Mucocutaneous Candidiasis (1x oral dose for vaginal candidiasis, IV for esophagitis)
- Cryptococcal meningitis (treatment and prophylaxis)
- Sepsis in ICU
- Skin and nails infections
List the second generation of triazoles.
- Ketoconazole
- Clotrimazole
- Imidazoles
- Posaconazole
- Voriconazole
What are the indications for Ketoconazole?
- For topical use in dermatophytos
- Can help in Cushing’s to ↓ cortisol production…due to the androgen/estrogen synthesis inhibition.
What are the indications for Clotrimazole?
Good for dermatophytosis and vaginal candidiasis topically.
What is important to remember about the imidazoles?
That they are not used systemically.
What are the indications of Posaconazole?
Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients.
What are the indications of Voriconazole?
- Invasive Aspergillosis
- Candida esophagitis (in AIDS patients)
What spectrum does Amphotericin B cover?
-
Broadest anti-fungal used for severe systemic fungal infections:
- Histo
- Coccidio
- Blasto
- Crypto meningitis (with flucytosine)
- Systemic candidiasis
- Works for all fungi except dermatophytes